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    • 4. 发明申请
    • Extended release formulation of beta-lactam antibiotics
    • β-内酰胺抗生素的延长释放制剂
    • US20060233878A1
    • 2006-10-19
    • US10568325
    • 2003-09-30
    • Shailesh BhamareIndu BhushanHimadri Sen
    • Shailesh BhamareIndu BhushanHimadri Sen
    • A61K31/545A61K9/22
    • A61K9/2018A61K9/2027A61K31/545
    • A pharmaceutical composition for controlled drug delivery comprising a β-lactam antibiotic or its pharmaceutically acceptable hydrates, salts or esters, and one or more carbomers. The above β-lactam antibiotics formulation avoids the limitations of known β-lactam controlled release form which are found to be either complex and/or cost-extensive to obtain requiring multiphase and/or selective coatings or fail to achieve the desired controlled release for once daily dosage form. Importantly, in the β-lactam antibiotic form of the above the rate-controlling polymer wherein the Cmax of the formulation is substantially the same as that of a single dose of the immediate release formulation. Also advantageously the formulation achieves a rate controlling polymer wherein the T>MIC for the formulation is more than 17 hours when the MIC is 0.25 mcg/ml and more than 10 hours when the MIC is 2 mcg/ml. The above β-lactam antibiotic form is thus directed to serve as the much desired simple and cost-effective controlled release form suitable for once daily administration.
    • 用于受控药物递送的药物组合物,其包含β-内酰胺抗生素或其药学上可接受的水合物,盐或酯,以及一种或多种卡波姆。 上述β-内酰胺抗生素制剂避免了已知的β-内酰胺控制释放形式的限制,其被认为是复杂的和/或成本广泛的以获得需要多相和/或选择性涂层或不能达到期望的一次控制释放 日剂量。 重要的是,在上述β-内酰胺抗生素形式中,速率控制聚合物,其中制剂的最大值与单剂量的立即释放制剂基本上相同。 还有利地,制剂实现速率控制聚合物,其中当MIC为0.25mcg / ml时,制剂的T> MIC大于17小时,当MIC为2mcg / ml时超过10小时。 因此,上述β-内酰胺抗生素形式被用作适合于每日一次给药的理想的简单和成本有效的控制释放形式。